JPH0259516A - Membrane stimulating action aromatic transmitting system - Google Patents

Abstract

PURPOSE: To provide a system for feeding of a medicine masking flavor of an activator and preventing gastric ulcer, comprising a flavor masking solid activator having an almost equal density to a suspended liquid and made to be hydrophilic. CONSTITUTION: This system is composed of beads an almost equal density to a suspended liquid and obtained by melting wax or preferably mono- and di-glyceride, mixing an activator and a flavor, a controller and/or air, as necessary, with the molten mixture, charging the resultant mixture in a spinner, discharging from the spinner as liquid beads and solidifying while cooling. A ratio of a masking film to the activator is adjusted to be able to reduce solubility of the activator during the first 60sec after the contact with the liquid. By the system, flavor can be masked in a solid administrating type, a liquid is administrated to a patient not digestible in the solid administrating type and a manifestation of gastric ulcer caused by quick dissolving can be avoided.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to aromatic drug delivery systems, and more particularly to the delivery of drugs that do not have a pleasant flavor or where ingestion in a solid state is undesirable. Those skilled in the art have expertise in flavor masking agents and related products.

BACKGROUND OF THE INVENTION The use of flavors to mask the taste of drugs is well known. However, flavor components are not sufficient to mask certain drugs and vitamins.

Therefore, physical methods of encapsulation and chemical barriers have been developed to mask its undesirable flavor characteristics.

Certain systems used in vitamins are eligible for U.S. Patent No. 3.
037911.3080292.3080293 and 3379994.

These methods produce products in beadlet form. Although these beadlets are effective at flavor masking, they can pose other problems with certain drugs and patient types.

For example, patients who have problems taking solid dosage forms may
Drugs produced by this beadlet method cannot be used.

Also, products such as potassium chloride are not effectively taken up in the beadlet form described in the prior art.

Potassium chloride in solid form is known to deposit along the lining of the stomach and intestines, causing ulcers in the lining of the stomach and intestines. This ulceration and bleeding related to the stomach is a highly undesirable side effect, especially for young patients. That is, the treatment of one disease is creating another serious medical problem.

The present invention is advantageous in that the flavor mask particles can be administered in liquid form. The present invention is also advantageous in that it allows for the production of products that are economical and exhibit commercially desirable properties.

Furthermore, the method of the invention is advantageous in that it does not affect the active properties of the administered drug. Other advantages include the ability to administer solid drug forms, particularly to patients who are unable to ingest large amounts of the drug. Finally, the method of the present invention solves a problem that has long been desired in the art.

SUMMARY OF THE INVENTION The drug delivery system of the present invention masks the flavor of an active agent;
Prevents stomach ulcers. The system consists of a taste-masking solid active agent made hydrophilic and having a density approximately equal to the carrier liquid to be clouded.

(Detailed Description of the Invention) The base particles are
92 3080293 and 3279994. The descriptions of these patents are incorporated herein by reference. Beads produced by these methods are hydrophobic and therefore unsuitable for formulation in L% E solutions.

Beads are formed by powdering the active agent. A preferred activator is potassium chloride powdered to 200 mt. The wax, preferably mono and nocricerit, is dissolved in a molten state. About glycerides
This is approximately 60-80°C. The activator is added to this molten mixture to make up 40-60% of the total volume.

Waxes and glycerides provide a flavor-masking coating on the active ingredients. In the present invention, the densities of the flavor masking coating and the active agent are approximately equal. The density of the entire product should be equal to the density of the liquid in which it is suspended.

That is, if the product is suspended in water, for example, its total density will be approximately l. Also, the flavor massaging membrane: active agent ratio should be adjusted such that drug solubility is reduced during the first 60 seconds.

Flavors, modifiers and/or air are added to the mixture. The mixture is placed in a spinner from which liquid beads of the mixture are discharged and allowed to solidify while cooling. Beads are usually 30 to 100 mesh. These can be compressed into tablet form.

The flavor masking coating is hydrophilic, so the beadlets float on water. In order to make the mixture hydrophilic or improve workability, a surfactant or a surface modifier is added to the mixture. A preferred surfactant is sodium lauryl sulfate, forming 0.25-2%, preferably 1% by weight of the beadlets. Surfactants can be added before or after spinning the beads.

Also, additional colorants and flavors can be added. Other materials can also be incorporated into the beads that do not impair the basic properties of the material. initially reduces solubility, but gastric acid p
It is particularly desirable to add pH regulators that are neutralized with H. This allows rapid dissolution in the stomach.

The beads can be packaged in single dose packages. If the patient needs to take a single dose, the white from the package is poured into a scoop of liquid. The beads are! 88 liquid and does not dissolve immediately.

However, it dissolves very quickly, 90% within 15 minutes, preventing gastric ulcers. The patient can drink the liquid.

The system of the present invention provides various advantages. First, the active ingredient can be flavor masked in solid dosage form.

Second, liquids can be administered to those who cannot ingest solid dosage forms. Third, it does not suffer from the side effects of solid dosage forms. Fourth, the rapid dissolution of the product prevents gastric ulcers. Fifth, we have succeeded in creating a delivery system that is more acceptable to consumption considerations, which complicates the needs of the patient when taking the drug, especially when large doses are required.

(Example) Next, the present invention will be explained in more detail by giving examples, but the present invention is not limited thereto.

Example 1 Albutyol Sulfate Modified Release Liquette A glue Liquette with the following composition was prepared.

Albutyrol Sulfate 7.5% Hydrogenated Vegetable Oil 92.5% Fat base was dissolved and albutyrol sulfate powder was carefully added.

The resulting melt was solidified in a spinning disk or other suitable spray solidification equipment.

The obtained beads were mixed with silicon dioxide and sodium lauryl sulfate to obtain glue kuetti with the following composition.

Albutyrol Sulfate Beads 99.25% Silicon Dioxide 0.25% Sodium Lauryl Sulfate 0.50% Example 2 Theophylline Release Controlled Lifuerati A glue kuetti with the following composition was prepared.

Theophylline 40% white wax
Dissolve the 60% wax base and carefully add the theophylline powder.

The resulting melt was solidified in a spinning disk or other suitable spray solidification equipment.

The obtained beads were mixed with silicon dioxide and sodium lauryl sulfate to obtain glue quetti having the following composition.

Theophylline Beads 99.25% Silicon Dioxide 0.25% Sodium Lauryl Sulfate 0.50% Example 3 Antacid Quetty Antacid Quetti consists of three separate types with the following compositions:

Bead #l Wt% Magnesium Hydroxide 21.31 Aluminum Hydroxide Dry Gel 2403 Na Azulene Sulfonate 0
．． 19 NaCu chlorophyllin 0.21 Mono and diglycerides 26.40 White wax
26.40 lauryl sulfate,
1.46100.00 Beads #2 Scopolia (S copol 1a) 10% Extract 60.00 Mono and Diglycerides 3990 FD&C Blue #1
0. 06FD & yellow #i5
0. 0□1100°00 Bead #3 Na Cu aa Fill: / 3.3.00 Stearic Acid 67.00 The base consisting of white wax, mono- and diglycerides, and stearic acid was melted and the active ingredient was carefully added.

The resulting melt was solidified in a spinning disk or other suitable spray solidification equipment.

The obtained beads were mixed at the following ratio.

Beads #l 13.5 parts Peas #2 beads #3 To the mixture, was remixed.

Silicon dioxide menthol, flavor peppermint, flavor sodium lauryl sulfate 2.01 and less than 10 parts of the mixture were added, and the total mixture was 50% 40% 07% 50% Patent source: K.V. Firman Uticals.
Incoholated

Claims (1)

Claims: 1. A drug delivery system comprising a taste-masking solid active agent rendered hydrophilic and having a density approximately the same as the carrier liquid in which it is suspended. 2. The flavor mask coating:active agent ratio is selected such that the solubility for about 60 seconds after contact with the liquid is less than that which allows the active agent to be tasted. System described in section. 3. The system of claim 1, wherein more than 90% of the flavor masking active agent dissolves within about 15 minutes after contact with the liquid. 4. The system according to claim 1, which contains a flavor. 5. The system of claim 1, comprising a surfactant to promote wetting. 6. The system of claim 1 containing a pH adjusting agent that initially reduces solubility but is neutralized by gastric acid pH. 7. Claim 1 in which the activator is calcium chloride
System described in section. 8. The system of claim 1, wherein the active agent is flavor masked by wax. 9. The system of claim 1, wherein the active agent is flavor masked by a mixture of mono- and diglycerides. 10. p to improve the physical/chemical stability of the system
2. The system of claim 1 containing an H modifier.